Molecular Aspects of the RT/drug Interactions. Perspective of Dual Inhibitors

Title:Molecular Aspects of the RT/drug Interactions. Perspective of Dual Inhibitors

Volume: 19 Issue: 10

Author(s): Simona Distinto, Elias Maccioni, Rita Meleddu, Angela Corona, Stefano Alcaro and Enzo Tramontano

Affiliation:

Keywords: HIV, RT binding pockets and novel inhibitors

Abstract: The HIV-1 reverse transcriptase (RT) is one of the most attracting targets for the development of early phase infection inhibitors. Although many RT inhibitors have been approved for the treatment of HIV-1 infection, they all target the polymerase function of this enzyme. So far, no drugs are available for the inhibition of the RT associated ribonuclease H function (RNase H), which plays an essential role in the HIV replication cycle. Moreover it should be reported that many of the known RT inhibitors, targeting the polymerase function, enhance the RNase H activity, indicating that, although spatially distinct, a close relation occurs between the two functions. The aim of this review is to summarise the efforts in the design of new inhibitors either characterized by a novel mechanism of action or capable of blocking both RT associated functions, as well as pointing out the main binding features of the known RT inhibitors.

Cite this article as:

Distinto Simona, Maccioni Elias, Meleddu Rita, Corona Angela, Alcaro Stefano and Tramontano Enzo, Molecular Aspects of the RT/drug Interactions. Perspective of Dual Inhibitors, Current Pharmaceutical Design 2013; 19 (10) . https://dx.doi.org/10.2174/1381612811319100009